BL 1249 - 98%, high purity , CAS No.18200-13-0, Activator of K 2P10.1;Activator of K 2P2.1

Item Number

B286784

• Synonyms: BL-1249|18200-13-0|BL 1249|1H-Tetrazole, 5-(o-((5,6,7,8-tetrahydro-1-naphthyl)amino)phenyl)-|5E7RR1J6TR|CHEMBL1417584|1-Naphthalenamine, 5,6,7,8-tetrahydro-N-[2-(2H-tetrazol-5-yl)phenyl]-|5,6,7,8-Tetrahydro-N-[2-(2H-tetrazol-5-yl)phenyl]-1-naphthalenamine
• Specifications & Purity: Moligand™, ≥98%
• Biochemical and Physiological Mechanisms: K2P2.1 (TREK-1) and K2P10.1 (TREK-2) channel opener (EC50values are 5.5 μM and 8 μM, respectively). Exhibits selectivity for bladder over vascular tissuein vitroandin vivo(EC50values are 1.26 and 21.0μM for cultured bladder and aortic tissues respectivel
• Storage Temp: Protected from light,Store at -20°C,Argon charged
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: ACTIVATOR
• Mechanism of action: Activator of K 2P10.1;Activator of K 2P2.1

Product Description

BL-1249 is a nonsteroidal anti-inflammatory agent (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM). 

Application：

BL-1249 has been used:
as an activator of mechano-gated K2P channel in contracted mouse ileum and colon tissues
as a TWIK related potassium channel (TREK2) modulator and in U-2 OS osteosarcoma cell line
as a TREK1 and TREK2 activator in mice.